Cancer is a disease seriously threatening human life. According to the statistics of WHO in 2008, people died of cancer in 2007 amounts to 7.9 million, which represents about 13% of all death tolls. Recently, with a deeper study into the tumorigenesis mechanism, the molecular mechanisms involving in the genesis and development of cancer are revealed gradually, and anti-tumor drugs have developed from initial cytotoxic drugs into tumor-specific targeted drugs.
Cell death can be divided into necrosis and programmed cell death, of which the most important type is apoptosis. Recent studies have revealed that the tumorigenesis and progression are resulted from not only uncontrolled cell proliferation and abnormal differentiation, but also imbalance of apoptosis. Apoptosis is a cell active death progress under the control of related genes which is triggered by a change of insider and outside environments or death signal, and can eliminate aged cells and potentially abnormal growing cells in vivo under physiological conditions. Therefore, it plays an important role in maintaining homeostasis in vivo. With a deeper study into the mechanism of apoptosis, many proteins have been identified to involve in apoptosis, including IAP family proteins, Smac/DIABLO protein, Bcl-2 family proteins, P53 gene, Proteasome proteinase, Caspase family proteins and so on.
Chemistry Professor Paul J. Hergenrother et al. at the University of Illinois found a small molecule compound PAC-1 by screening more than 20000 compounds with different structures. PAC-1 could activate Procaspase-3 directly and induce the apoptosis of cancer cells. Studies showed that PAC-1 could activate Procaspase-3 significantly both in vitro and in vivo, and cancer cells would be also induced to apoptosis within 23 hours after treatment with PAC-1.

Based on the references, the inventor designs and synthesizes a serial of substituted hydrazide compounds, which are shown to possess a strong antitumor activity and little side effect by in vitro screening assay for antitumor activity on various tumor cell strains.